Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2,3 or 4; X is --C(.dbd.O)-- or --(CH.sub.2).sub.m --, in which m is the integer 0 or 1; Y is methylene, ethylene or ethenylene, or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;X represents oxa or thia;Y represents H or hydroxy;R.sup.1 and R.sup.2 independently represent phenyl or thienyl, either of which groups may be optionally substituted by halo or trifluoromethyl;R.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SCH.sub.3, SOCH.sub.3, SO.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;R.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl,are tachykinin antagonists. They and compositions thereof are therefore useful in therapy.

Abstract: This invention provides novel 3-quinuclidinyl benzamides and benzoates which have utility as therapeutical agents which exhibit anxiolytic, antipsychotic, cognition improvement, antiemetic and gastric prokinetic effects in warm blooded animals.The compounds useful in the methods and composition of this invention are represented by the formula: ##STR1## where X is oxygen or sulfur; Y is --NH or --O--; when Y is --O--, R.sup.1 is ##STR2## and when Y is --NH, R.sup.1 is ##STR3## and R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkenyl; the geometrical and optical isomers, or a pharmaceutically acceptable salt thereof.

Abstract: A quinoline derivative of the formula (I): ##STR1## wherein each phenyl ring of A, B and C can have one or more substituents, X is ##STR2## (R.sup.1 is a hydrogen atom or a lower alkyl group) or ##STR3## (R.sup.2 is a lower alkyl group or a lower alkoxy group), and n is 0 or 1, or its salt, which possesses an inhibitory action against acyl-CoA: cholesterol acyltransferase.

Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.

Abstract: Disclosed is pyrazoloacridone derivatives represented by formula (I): ##STR1## wherein: each of R.sup.1a, R.sup.1b, R.sup.1c and R.sup.1d independently represents hydrogen, lower alkyl, --(CH.sub.2).sub.p --Xwherein p represents an integer of 1 to 6, and X represents hydroxy, lower alkoxy or --NR.sup.2a R.sup.2bwherein each of R.sup.2a and R.sup.2b independently represents hydrogen, lower alkyl, or --(CH.sub.2).sub.m --Ywherein m represents an integer of 1 to 6, and Y represents hydroxy, lower alkoxy or --NR.sup.3a R.sup.3bwherein each of R.sup.3a and R.sup.3b independently represents hydrogen or lower alkylor --CH[(CH.sub.2).sub.n OH].sub.2wherein n represents an integer of 1 to 5; or a pharmaceutically acceptable salt thereof.

Abstract: A compound of formula (I) useful for treating dementia or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents Z, where Z is a group in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises two or three nitrogen atoms, any amino nitrogen being substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, r represents the integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0, with the proviso that when Y is hydrogen s is 1.

Abstract: Polyoxoheterocyclic tetracycles related to the Chinese antimalarial natural product qinghaosu (artemisinin) are disclosed. These materials have a ##STR1## core structure with an oxygen (carbonyl or alkyl ether) at position 12 and in some cases one or two alkyl or aralkyl substituents at position 11. These materials have antimalarial properties.

Abstract: Azabicyclo[2.2.2]octan-3-imines of the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein are prepared by reacting a compound of the formula ##STR2## ps with a compound of the formula wherein A is MgCl, MgBr or Li.

Abstract: The invention relates to new compounds of formula I: ##STR1## in which: m represents zero, 1, 2, 3 or 4,n and p represent zero, 1 or 2,W represents an oxygen atom, an --NH-- radical, or a single bond,R represents a 4-oxo-4H-chromen-2-yl radical,R.sub.1 represents a hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, or an aryl radical, andR.sub.2 represents a hydrogen atom, an alkyl radical, an alkenyl radical, a cycloalkyl radical, a benzyl radical, a phenyl radical, an aralkyl radical, an alkoxyalkyl radical or a polyhalogenated alkyl radical, the optical isomers thereof and the addition salts thereof with a pharmaceutically acceptable organic or mineral acid,and medicaments containing the same, are disclosed.

Abstract: There are described compounds of the formula ##STR1## where A is CH or N;X is hydrogen, loweralkyl, halogen, trifluromethyl, loweralkoxy, arylloweralkoxy, hydroxy or phenylamino;Y is hydrogen, loweralkyl, halogen, loweralkoxy, arylloweralkoxy or hydroxy;R.sub.1 is hydrogen or loweralkyl;R.sub.2 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl or aryloxycarbonyl;R.sub.3 is hydrogen, alkyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ;which compounds are useful as topical antiinflammatory agents for the treatment of skin disorders.

Abstract: The present invention is 3,5-substituted, isoxazoles, pyrazoles, isothiazoles, and analogs thereof having 5-lipoxygenase or cyclooxygenase inhibiting activity or as a sunscreen.

Abstract: The present invention provides compounds of the formula (I): ##STR1## wherein R is a phenyl group, substituted fluorine atoms formulations containing them and their use in controlling pest infestation.

Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a pyridyl, group; X is halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azido, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl; Y and Z are each independently a hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azido, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytophthogenic fungi.

Abstract: Methods and compositions for blocking various channels and receptors within an organism are provided. For example, two toxins were isolated from the Agelenopsis aperta spider. The first toxin comprised a toxin having a molecular weight of from aproximately 5,000 to approximately 10,000. This toxin was found to have an irreversible effect on calcium channels within the central nervous system. A second toxin having a molecular weight of less than about 1,000 was also isolated. This toxin was found to have a reversible blocking effect on calcium channels within the central nervous system and the cardiovascular system.A third toxin was isolated from the Argiope aurantia spider. This toxin was found to have a reversible effect on excitatory amino acid receptors. Finally, a toxin having a molecular weight of from approximately 5,000 to approximately 7,000 daltons was isolated from the Hololena curta spider. This toxin was found to have an irreversible effect on excitatory amino acid receptors.

Abstract: The present invention is directed to a class of 3-phosphono-piperidine and pyrrolidine derivatives and their use as NMDA antagonists.

Abstract: The invention relates to new compounds of formula I: ##STR1## in which: m represents zero, 1, 2, 3 or 4,n and p represent zero, 1 or 2,W represents an oxygen atom, an --NH-- radical, or a single bond,R represents a benzocyclobuten-1-yl radical, or an indanyl radical, a 2,3-dihydrobenzofuran-2-ylR.sub.1 represents a hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, or an aryl radical, andR.sub.2 represents a hydrogen atom, an alkyl radical, an alkenyl radical, a cycloalkyl radical, a benzyl radical, a phenyl radical, an aralkyl radical, an alkoxyalkyl radical or a polyhalogenated alkyl radical, the optical isomers thereof and the addition salts thereof with a pharmaceutically acceptable organic or mineral acid, and medicaments containing the same.

Abstract: New substituted urea compounds of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## whereinA is ##STR2## wherein R.sup.3 is an oxadiazol, substituted with C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 alkynyl, C.sub.3-7 cycloalkyl, benzyl, phenyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, amino or alkylamino;R.sup.2 is --H or lower alkyl;X is O or S; andR.sup.1 is a group of formula II, III, IV or V ##STR3## where n is 2 or 3, p is 1 or 2, q is 1 to 3, r is 1-3 and R.sup.4 and R.sup.5 are H, C.sub.1-7 alkyl or C.sub.3-6 cycloalkyl; and N-oxides thereof.The compounds are useful in pharmaceutical preparations for treating psychotic disorders, nausea and vomiting.

Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,R.sub.1 and R.sub.2, identical or different, represent hydrogen, a linear, branched or cyclic alkyl, alkenyl, or alkynyl which contain up to 6 carbon atoms, R.sub.1 and R.sub.2 optionally substituted by hydroxy, alkoxy containing up to 6 carbon atoms, aralkyl containing up to 14 carbon atoms, a COOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, a --CON(alk.sub.2).sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon atoms, the radical --C(R.sub.1).dbd.NOR.sub.2 being in position 2, 3 or 4, in all their isomer forms and their mixture, as well as their addition salts with pharmaceutically acceptable organic or mineral acids. Also therapeutic compositions containing the compound, method of treatment and method of preparation.

Abstract: Disclosed is a process for the preparation of hindered amine light stabilizers by reacting (a) an alkyl substituted-4-hydroxypiperidine with (b) a dicarboxylic acid ester, in the presence of a catalyst system comprising a basic inorganic compound and a polar aprotic organic compound.